Compounds for preventing, reducing and/or alleviating itchy skin condition(s)

Abstract

The present invention primarily relates to the use of one or more specific compounds and/or one or more respective salt(s) thereof for preventing, reducing or alleviating itchy skin condition(s), and/or as PAR-2 antagonist. Furthermore, the present invention relates to compositions (products or, respectively, formulations), in particular for topical administration, preferably cosmetic or pharmaceutical compositions, in particular for preventing, reducing or alleviating one or more itchy skin conditions and/or for providing a PAR-2 antagonistic effect, comprising or consisting of an effect amount of such compound(s) and/or salt(s) and one or more cosmetically and/or pharmaceutically acceptable carriers.

1 - 18 . (canceled) 
     
     
         19 . A method for preventing, reducing or alleviating itchy skin conditions comprising administering to an individual in need thereof a compound of formula 1 or a salt thereof: 
       
         
           
           
               
               
           
         
         wherein, R1, R2, R3 and R4 are independently selected from —OH, —OR or —OCOR; 
         R is an alkyl group comprising 1-12 carbon atoms; and 
         X is —H or —OH. 
       
     
     
         20 . The method according to  claim 19 , wherein the compound has a structure according to formula 2 or a salt thereof: 
       
         
           
           
               
               
           
         
         Wherein, R1, R2, R3 and R4 and X are as defined in  claim 19 . 
       
     
     
         21 . The method according to  claim 19 , wherein the compound has a structure according to formula 3 or a salt thereof: 
       
         
           
           
               
               
           
         
       
     
     
         22 . The method according to  claim 19 , wherein the compound has a structure according to formula 4 or a salt thereof: 
       
         
           
           
               
               
           
         
       
     
     
         23 . The method according to  claim 19 , further comprising administering one or more substances selected from the group consisting of:
 (i) anti-itch compounds,   (ii) steroidal anti-inflammatory substances of the corticosteroid type,   (iii) non-steroidal anti-inflammatory substances,   (iv) natural or naturally occurring anti-inflammatory substances or substances that alleviate reddening and/or itching,   (v) alpha-bisabolol, apigenin, apigenin-7-glucoside, gingerols, shogaols, gingerdiols, dehydrogingerdiones, paradols, natural avenanthramides, non-natural avenanthramides, preferably dihydroavenanthramide D, boswellic acid, phytosterols, glycyrrhizin, glabridin and licochalcone A,   (vi) skin care agents,   (vii) physiological cooling agents, and   (viii) histamine receptor antagonists, serine protease inhibitors, TRPV1 antagonists, NK1 antagonists, cannabinoid receptor agonists and TRPV3 antagonists.   
     
     
         24 . The method according to  claim 19 , wherein said one or more compounds of formula 1 and/or salt(s) thereof is present in an amount sufficient to prevent, reduce or alleviate one or more itchy skin conditions. 
     
     
         25 . The method according to  claim 19 , wherein the compound(s) and/or salt(s) thereof, is applied to skin, and remains on the skin for at least 5 minutes. 
     
     
         26 . A method for antagonizing PAR-2 in an individual in need thereof comprising administering a compound of formula 1 or a salt thereof: 
       
         
           
           
               
               
           
         
         wherein, R1, R2, R3 and R4 are independently selected from —OH, —OR or —OCOR; 
         R is an alkyl group comprising 1-12 carbon atoms; and 
         X is —H or —OH. 
       
     
     
         27 . The method according to  claim 26 , wherein the compound has a structure according to formula 2 or a salt thereof: 
       
         
           
           
               
               
           
         
         wherein R1, R2, R3 and R4 and X are as defined in  claim 26 . 
       
     
     
         28 . The method according to  claim 26 , wherein the compound has a structure according to formula 3 or a salt thereof: 
       
         
           
           
               
               
           
         
       
     
     
         29 . The method according to  claim 26 , wherein the compound has a structure according to formula 4 or a salt thereof: 
       
         
           
           
               
               
           
         
       
     
     
         30 . The method according to  claim 26 , wherein the composition comprising the compound(s) and/or salt(s) thereof, is applied to skin, and remains on the skin for at least 5 minutes. 
     
     
         31 . A composition comprising:
 a) from 0.01 to 10.0 wt. %, based on the total weight of said composition, of one or more compounds according to formula 1:   
       
         
           
           
               
               
           
         
         Wherein, R1, R2, R3 and R4 are independently selected from —OH, —OR or —OCOR; 
         R is an alkyl group comprising 1-12 carbon atoms; and 
         X is —H or —OH, and 
         b) one or more cosmetically and/or pharmaceutically acceptable carriers. 
       
     
     
         32 . The composition according to  claim 31 , wherein the compound has a structure according to formula 2 or a salt thereof: 
       
         
           
           
               
               
           
         
         wherein R1, R2, R3 and R4 and X are as defined in  claim 31 . 
       
     
     
         33 . The composition according to  claim 31 , wherein the compound has a structure according to formula 3 or a salt thereof: 
       
         
           
           
               
               
           
         
       
     
     
         34 . The composition according to  claim 31 , wherein the compound has a structure according to formula 4 or a salt thereof: 
       
         
           
           
               
               
           
         
       
     
     
         35 . The composition according to  claim 31 , wherein the cosmetically and/or pharmaceutically acceptable carrier(s) comprise one or more of:
 (i) polyethylene glycol esters of formula 5   
       
         
           
           
               
               
           
         
         
           wherein m is an integer from 3-7, 
           R1 is H or 
         
       
       
         
           
           
               
               
           
         
          and
 R2 is a branched or unbranched alkyl group, 
 
         (ii) polyethyleneglycol ethers of formula 6
   R 3 OCH 2 —CH 2  n OR 4   (formula 6)
 
 wherein m is an integer from 7-30, and 
 R3 and R4 are independently H or a saturated or unsaturated, branched or unbranched alkyl group, 
 
         (iii) (alkane) diols having 3 to 10 carbon atoms, 
         (iv) esters having 6 to 36 carbon atoms, 
         (v) branched and unbranched alkyl or alkenyl alkohols, 
         (vi) branched and unbranched hydrocarbons and waxes, cyclic or linear silicone oils and dialkyl ethers having 6 to 24 carbon atoms, and 
         (vii) solvents selected from the group consisting of acetone, methylpropyl ketone, dipropyl ketone, dimethyl sulfoxide, glycerine carbonate, propylene carbonate, butylene carbonate, glycerine formal, solketal, 2-etyhl hexanol, 2-butyl octanol, 2-hexyl decanol and 2-octyl dodecanol. 
       
     
     
         36 . The composition according to  claim 31 , further comprising one or more substances selected from the group consisting of:
 (i) anti-itch compounds,   (ii) steroidal anti-inflammatory substances of the corticosteroid type,   (iii) non-steroidal anti-inflammatory substances,   (iv) natural or naturally occurring anti-inflammatory substances or substances that alleviate reddening and/or itching,   (v) alpha-bisabolol, apigenin, apigenin-7-glucoside, gingerols, shogaols, gingerdiols, dehydrogingerdiones, paradols, natural avenanthramides, non-natural avenanthramides, preferably dihydroavenanthramide D, boswellic acid, phytosterols, glycyrrhizin, glabridin and licochalcone A,   (vi) skin care agents,   (vii) physiological cooling agents, and   (viii) histamine receptor antagonists, serine protease inhibitors, TRPV1 antagonists, NK1 antagonists, cannabinoid receptor agonists or TRPV3 antagonists.   
     
     
         37 . The composition according  claim 31 , further comprising one or more substances selected from the groups consisting of:
 extracts or fractions from camomile,  Aloe vera , oats, calendula,  arnica , honeysuckle, rosemary, witch hazel, ginger or  Echinacea , alpha-bisabolol, gingerols, shogaols, gingerdiols, dehydrogingerdiones, paradols, natural avenanthramides, non-natural avenanthramides, preferably dihydroavenanthramide D, boswellic acid, phytosterols, glycyrrhizin, and licochalcone A, urea, hyaluronic acid, allantoin, panthenol, lanolin, alpha-hydroxy acids (preferably citric acid, lactic acid), vitamin E and derivatives thereof.   
     
     
         38 . The composition according to  claim 31 , wherein the composition is in the form of alcoholic or aqueous/alcoholic solution, dispersion, suspension, emulsion, ointment, paste, gel, balm, serum, powder, wipe, Eau de Toilette, Eau de Cologne, perfume, stick, roll-on, (pump) spray, aerosol, leave-on skin care composition, leave-on insect repellent composition, sunscreen composition, skin-lightening composition, self-tanning composition, aftersun preparation, shaving or after-shave composition, hair-removing composition, hair care composition, preferably conditioner, hair lotion, hair tonic, styling cream, pomade, styling aid, permanent wave and fixing compositions, hair smoothing composition, hair straightening composition, hair relaxer, hair setting composition, blonding composition, hair coloring composition, such as e.g. temporary, directly absorbed, semi-permanent hair coloring composition, permanent hair coloring composition, decorative cosmetic composition, deodorant and/or antiperspirant composition. 
     
     
         39 . A pharmaceutical composition comprising:
 (i) from 0.01 to 10 wt. % based on the total weight of said composition, one or more compounds according to formula 1:   
       
         
           
           
               
               
           
         
         wherein R1, R2, R3 and R4 are independently selected from —OH, —OR or —OCOR; 
         R is an alkyl group comprising 1-12 carbon atoms; and 
         X is —H or —OH; and 
         (ii) a pharmaceutically acceptable carrier. 
       
     
     
         40 . The pharmaceutical composition according to  claim 39 , wherein the compound has a structure according to formula 2 or a salt thereof: 
       
         
           
           
               
               
           
         
         wherein R1, R2, R3 and R4 and X are as defined in  claim 39 . 
       
     
     
         41 . The pharmaceutical composition according to  claim 39 , wherein the compound has a structure according to formula 3 or a salt thereof: 
       
         
           
           
               
               
           
         
       
     
     
         42 . The pharmaceutical composition according to  claim 39 , wherein the compound has a structure according to formula 4 or a salt thereof: 
       
         
           
           
               
               
           
         
       
     
     
         43 . The pharmaceutical composition according to  claim 39 , wherein said one or more compound(s) of formula 1 and/or salt(s) thereof is present in an amount sufficient to a) prevent, reduce or alleviate one or more itchy skin conditions, and/or to b) provide a PAR-2 antagonistic effect.